EP0760654A1 - Process for producing active agent preparations in the form of a solid solution of the active agent in a polymer matrix and active agent preparations obtained thereby - Google Patents
Process for producing active agent preparations in the form of a solid solution of the active agent in a polymer matrix and active agent preparations obtained therebyInfo
- Publication number
- EP0760654A1 EP0760654A1 EP96907439A EP96907439A EP0760654A1 EP 0760654 A1 EP0760654 A1 EP 0760654A1 EP 96907439 A EP96907439 A EP 96907439A EP 96907439 A EP96907439 A EP 96907439A EP 0760654 A1 EP0760654 A1 EP 0760654A1
- Authority
- EP
- European Patent Office
- Prior art keywords
- active agent
- active ingredient
- preparations
- active
- active substance
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
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- 239000013543 active substance Substances 0.000 title claims abstract description 41
- 238000002360 preparation method Methods 0.000 title claims abstract description 26
- 229920000642 polymer Polymers 0.000 title claims abstract description 23
- 239000006104 solid solution Substances 0.000 title claims abstract description 18
- 239000011159 matrix material Substances 0.000 title claims abstract description 10
- 150000003839 salts Chemical class 0.000 claims abstract description 25
- 239000004480 active ingredient Substances 0.000 claims description 48
- 229920003169 water-soluble polymer Polymers 0.000 claims description 8
- 229920001577 copolymer Polymers 0.000 claims description 5
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 3
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- 239000003381 stabilizer Substances 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 239000012085 test solution Substances 0.000 description 1
- 239000011573 trace mineral Substances 0.000 description 1
- 235000013619 trace mineral Nutrition 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 239000001069 triethyl citrate Substances 0.000 description 1
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 1
- 235000013769 triethyl citrate Nutrition 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 238000000870 ultraviolet spectroscopy Methods 0.000 description 1
- 229960001722 verapamil Drugs 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
- B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
- B01J2/00—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic
- B01J2/20—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic by expressing the material, e.g. through sieves and fragmenting the extruded length
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Processes Of Treating Macromolecular Substances (AREA)
- Compositions Of Macromolecular Compounds (AREA)
Abstract
Description
Claims
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19509807A DE19509807A1 (en) | 1995-03-21 | 1995-03-21 | Process for the preparation of active substance preparations in the form of a solid solution of the active substance in a polymer matrix, and active substance preparations produced using this method |
DE19509807 | 1995-03-21 | ||
PCT/EP1996/001047 WO1996029061A1 (en) | 1995-03-21 | 1996-03-12 | Process for producing active agent preparations in the form of a solid solution of the active agent in a polymer matrix and active agent preparations obtained thereby |
Publications (2)
Publication Number | Publication Date |
---|---|
EP0760654A1 true EP0760654A1 (en) | 1997-03-12 |
EP0760654B1 EP0760654B1 (en) | 2001-08-16 |
Family
ID=7757018
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP96907439A Expired - Lifetime EP0760654B1 (en) | 1995-03-21 | 1996-03-12 | Process for producing active agent preparations in the form of a solid solution of the active agent in a polymer matrix |
Country Status (18)
Country | Link |
---|---|
US (1) | US5741519A (en) |
EP (1) | EP0760654B1 (en) |
JP (1) | JP4017661B2 (en) |
KR (1) | KR970703133A (en) |
CN (1) | CN1081458C (en) |
AT (1) | ATE204162T1 (en) |
AU (1) | AU5106996A (en) |
BR (1) | BR9605886A (en) |
CA (1) | CA2190882C (en) |
CZ (1) | CZ340596A3 (en) |
DE (2) | DE19509807A1 (en) |
ES (1) | ES2163008T3 (en) |
HU (1) | HUP9603530A3 (en) |
IL (1) | IL117532A0 (en) |
MX (1) | MX9605678A (en) |
NO (1) | NO313485B1 (en) |
WO (1) | WO1996029061A1 (en) |
ZA (1) | ZA962243B (en) |
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US8323889B2 (en) | 2004-07-01 | 2012-12-04 | Gruenenthal Gmbh | Process for the production of an abuse-proofed solid dosage form |
US8383152B2 (en) | 2008-01-25 | 2013-02-26 | Gruenenthal Gmbh | Pharmaceutical dosage form |
US8722086B2 (en) | 2007-03-07 | 2014-05-13 | Gruenenthal Gmbh | Dosage form with impeded abuse |
US9161917B2 (en) | 2008-05-09 | 2015-10-20 | Grünenthal GmbH | Process for the preparation of a solid dosage form, in particular a tablet, for pharmaceutical use and process for the preparation of a precursor for a solid dosage form, in particular a tablet |
US9636303B2 (en) | 2010-09-02 | 2017-05-02 | Gruenenthal Gmbh | Tamper resistant dosage form comprising an anionic polymer |
US9655853B2 (en) | 2012-02-28 | 2017-05-23 | Grünenthal GmbH | Tamper-resistant dosage form comprising pharmacologically active compound and anionic polymer |
US9675610B2 (en) | 2002-06-17 | 2017-06-13 | Grünenthal GmbH | Abuse-proofed dosage form |
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US10058548B2 (en) | 2003-08-06 | 2018-08-28 | Grünenthal GmbH | Abuse-proofed dosage form |
US10064945B2 (en) | 2012-05-11 | 2018-09-04 | Gruenenthal Gmbh | Thermoformed, tamper-resistant pharmaceutical dosage form containing zinc |
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US10154966B2 (en) | 2013-05-29 | 2018-12-18 | Grünenthal GmbH | Tamper-resistant dosage form containing one or more particles |
US10201502B2 (en) | 2011-07-29 | 2019-02-12 | Gruenenthal Gmbh | Tamper-resistant tablet providing immediate drug release |
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US10449547B2 (en) | 2013-11-26 | 2019-10-22 | Grünenthal GmbH | Preparation of a powdery pharmaceutical composition by means of cryo-milling |
US10624862B2 (en) | 2013-07-12 | 2020-04-21 | Grünenthal GmbH | Tamper-resistant dosage form containing ethylene-vinyl acetate polymer |
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-
1995
- 1995-03-21 DE DE19509807A patent/DE19509807A1/en not_active Withdrawn
-
1996
- 1996-03-12 US US08/737,745 patent/US5741519A/en not_active Expired - Lifetime
- 1996-03-12 WO PCT/EP1996/001047 patent/WO1996029061A1/en active IP Right Grant
- 1996-03-12 DE DE59607490T patent/DE59607490D1/en not_active Expired - Lifetime
- 1996-03-12 BR BR9605886A patent/BR9605886A/en not_active Application Discontinuation
- 1996-03-12 CA CA002190882A patent/CA2190882C/en not_active Expired - Lifetime
- 1996-03-12 AT AT96907439T patent/ATE204162T1/en not_active IP Right Cessation
- 1996-03-12 KR KR1019960706601A patent/KR970703133A/en not_active Application Discontinuation
- 1996-03-12 EP EP96907439A patent/EP0760654B1/en not_active Expired - Lifetime
- 1996-03-12 HU HU9603530A patent/HUP9603530A3/en unknown
- 1996-03-12 MX MX9605678A patent/MX9605678A/en not_active IP Right Cessation
- 1996-03-12 AU AU51069/96A patent/AU5106996A/en not_active Abandoned
- 1996-03-12 ES ES96907439T patent/ES2163008T3/en not_active Expired - Lifetime
- 1996-03-12 CN CN96190364A patent/CN1081458C/en not_active Expired - Lifetime
- 1996-03-12 CZ CZ963405A patent/CZ340596A3/en unknown
- 1996-03-12 JP JP52804396A patent/JP4017661B2/en not_active Expired - Lifetime
- 1996-03-18 IL IL11753296A patent/IL117532A0/en unknown
- 1996-03-20 ZA ZA9602243A patent/ZA962243B/en unknown
- 1996-11-20 NO NO19964939A patent/NO313485B1/en not_active IP Right Cessation
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US10058548B2 (en) | 2003-08-06 | 2018-08-28 | Grünenthal GmbH | Abuse-proofed dosage form |
US8114383B2 (en) | 2003-08-06 | 2012-02-14 | Gruenenthal Gmbh | Abuse-proofed dosage form |
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US10729658B2 (en) | 2005-02-04 | 2020-08-04 | Grünenthal GmbH | Process for the production of an abuse-proofed dosage form |
US10675278B2 (en) | 2005-02-04 | 2020-06-09 | Grünenthal GmbH | Crush resistant delayed-release dosage forms |
US8722086B2 (en) | 2007-03-07 | 2014-05-13 | Gruenenthal Gmbh | Dosage form with impeded abuse |
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Also Published As
Publication number | Publication date |
---|---|
CZ340596A3 (en) | 1997-06-11 |
CN1150757A (en) | 1997-05-28 |
NO313485B1 (en) | 2002-10-14 |
AU5106996A (en) | 1996-10-08 |
CN1081458C (en) | 2002-03-27 |
DE59607490D1 (en) | 2001-09-20 |
NO964939D0 (en) | 1996-11-20 |
ATE204162T1 (en) | 2001-09-15 |
WO1996029061A1 (en) | 1996-09-26 |
NO964939L (en) | 1997-01-17 |
ZA962243B (en) | 1997-09-22 |
HU76547A2 (en) | 1997-09-29 |
US5741519A (en) | 1998-04-21 |
IL117532A0 (en) | 1996-07-23 |
JPH10501000A (en) | 1998-01-27 |
HUP9603530A3 (en) | 2001-12-28 |
CA2190882A1 (en) | 1996-09-26 |
HU9603530D0 (en) | 1997-02-28 |
KR970703133A (en) | 1997-07-03 |
MX9605678A (en) | 1998-04-30 |
ES2163008T3 (en) | 2002-01-16 |
JP4017661B2 (en) | 2007-12-05 |
BR9605886A (en) | 1997-09-16 |
DE19509807A1 (en) | 1996-09-26 |
EP0760654B1 (en) | 2001-08-16 |
CA2190882C (en) | 2007-01-16 |
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